Budesonide-loaded nanostructured lipid carriers reduce inflammation in murine DSS-induced colitis

被引：125
作者：
Beloqui, Ana [1 ,2 ,3 ]
Coco, Regis [3 ]
Alhouayek, Mireille [4 ,5 ]
Angeles Solinis, Maria [1 ,2 ]
Rodriguez-Gascon, Alicia [1 ,2 ]
Muccioli, Giulio G. [4 ]
Preat, Veronique [3 ]
机构：
[1] Univ Basque Country, UPV EHU, Sch Pharm, Pharmacokinet Nanotechnol & Gene Therapy Grp, Vitoria, Spain
[2] Univ Basque Country, UPV EHU, Ctr Invest Lascaray Ikergunea, Vitoria, Spain
[3] Catholic Univ Louvain, Louvain Drug Res Inst, B-1200 Brussels, Belgium
[4] Catholic Univ Louvain, Louvain Drug Res Inst, Bioanal & Pharmacol Bioact Lipids Res Grp, B-1200 Brussels, Belgium
[5] Catholic Univ Louvain, Louvain Drug Res Inst, Med Chem Res Grp, B-1200 Brussels, Belgium
来源：
INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2013年 / 454卷 / 02期
关键词：
Nanostructured lipid carriers; Macrophages; Colonic delivery; Inflammatory bowel disease; Budesonide; BOWEL-DISEASE; DRUG-DELIVERY; COLON; LIPOPOLYSACCHARIDE; MICROPARTICULATE; PATHOGENESIS; LIPOSOMES; RAT;
D O I：
10.1016/j.ijpharm.2013.05.017
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The challenge for the treatment of inflammatory bowel disease (IBD) is the delivery of the drug to the site of inflammation. Because nanoparticles have the ability to accumulate in inflamed regions, the aim of the present study was to evaluate nanostructured lipid carriers (NLCs) as nanoparticulate drug delivery systems for the treatment of IBD. Budesonide (BDS) was chosen as a candidate anti-inflammatory drug. BDS-loaded NLCs (BDS-NLC) produced by high-pressure homogenization had a size of 200 nm and a negative zeta potential. BDS-NLCs reduced the TNF-alpha secretion by activated macrophages (J774 cells). BDS-NLCs were more active in a murine model of dextran sulfate-induced colitis when compared with Blank-NLCs or a BDS suspension: BDS-NLCs decreased neutrophil infiltration, decreased the levels of the pro-inflammatory cytokines IL-1 beta and TNF-alpha in the colon and improved the histological scores of the colons. These data suggest that NLCs could be a promising alternative to polymeric nanoparticles as a targeted drug delivery system for IBD treatment. (C) 2013 Elsevier B. V. All rights reserved.
引用
收藏
页码：775 / 783
页数：9
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